关白附薄膜包衣片的处方和制备工艺研究

目的:研制关白附薄膜包衣片,为临床提供服用方便、疗效明显的抗房颤口服新药。方法:使用新型的直接压片辅料,筛选可压性和流动性良好的处方,运用全粉末直接压片技术制备关白附总碱盐片,并对其进行薄膜包衣。结果:优化后的处方流动性良好,片剂外观色泽均匀,硬度、片重差异、崩解时限等指标均符合《中华人民共和国药典》2010年版的要求,包衣后药物的引湿性有明显的改善。结论:采用全粉末压片技术制备关白附总碱盐片并用欧巴代进行包衣,有效地降低了药物的吸湿性,该工艺操作简单可行,适合工业化生产。     

不同处方因素对替硝唑口腔生物黏附片性能的影响

目的制备替硝唑口腔生物黏附片,并探讨不同处方因素对其性能的影响.方法选择不同规格的Carbopol和HPMC作为黏膜黏附材料和缓释骨架材料,用直接粉末压片法制备替硝唑口腔黏附片.考察不同处方因素对黏附片的黏附力、体外溶胀率和体外释药速率等性能的影响.结果随着Carbopol用量的增加,黏附片的黏附力、体外溶胀率呈现增加的趋势.通过体外释放度结果表明TNZ口腔黏附片存在着不同的释药机制.结论不同规格和用量的Carbopol和HPMC影响黏附片的性能.     

The effect of some formulation and process variables on the surface roughness of film-coated tablets

The effect of some formulation and process variables on the surface appearance of film-coated tablets has been examined by measuring the arithmetic mean roughness, Ra, values across the faces of tablets before and after they were coated with hydroxypropyl methyl-cellulose. For all tablet cores except those that were very porous, film coating resulted in an increasing surface roughness; for very porous cores a decrease was found. Tablets with rough surfaces were produced by coating with low molecular weight grades of the polymer; increaseing the polymer molecular weight resulted in a smoother finish with a minimum roughness at intermediate molecular weight grades. Increasing the polymer concentration above 2% w/v caused an increase in roughness as did increasing film thickness to 140 μm. There was a minimum in roughness at film thicknesses of 20 μm. The addition of pigment in low concentrations (0–25% v/v) caused a marginal increase in surface roughness but at concentrations above the critical pigment volume concentration, the surfaces were very rough. The results illustrate the potential of the method in the optimization of film formulations and process conditions during product development.     

The effect of some formulation and process variables on the surface roughness of film-coated tablets.

The effect of some formulation and process variables on the surface appearance of film-coated tablets has been examined by measuring the arithmetic mean roughness, Ra, values across the faces of tablets before and after they were coated with hydroxypropyl methyl-cellulose. For all tablet cores except those that were very porous, film coating resulted in an increasing surface roughness; for very porous cores a decrease was found. Tablets with rough surfaces were produced by coating with low molecular weight grades of the polymer; increasing the polymer molecular weight resulted in a smoother finish with a minimum roughness at intermediate molecular weight grades. Increasing the polymer concentration above 2% w/v caused an increase in roughness as did increasing film thickness to 140 micrometer. There was a minimum in roughness at film thickness of 20 micrometer. The addition of pigment in low concentrations (0--25% v/v) caused a marginal increase in surface roughness but at concentrations above the critical pigment volume concentration, the surfaces were very rough. The results illustrate the potential of the method in the optimization of film formulations and process conditions during product development.     

咪唑斯汀缓释片的处方工艺筛选

目的：制备一种能在5h内完全释放的咪唑斯汀缓释片。方法：以体外释放度的测定为主要考察指标，采用单因素筛选法，初步确定缓释片的处方，再对处方进一步的优化调整，确定处方中各辅料的用料量，并对缓释片的工艺在常规方法的基础上进行各项参数的优选，最后将自制缓释片与国外上市产品进行各项体外指标的对比试验。结果：其1000片配方为咪唑斯汀10mg、羟丙甲纤维素（HPMC）11．5mg、酒石酸氢钾40mg、乳糖110mg、微晶纤维素40mg、10％的乙基纤维素（EC）乙醇溶液0．068mL。结论：该处方工艺制备的咪唑斯汀缓释片能达到5h缓释的预期要求，达到了国外该制剂的同等水平，经验证适合扩大生产。     

The influence of compression and formulation on the hardness, disintegration, dissolution, absorption and excretion of sulphadimidine tablets

Sulphadimidine tablets were prepared with different binding agents and compressed at different compression levels, ranging from 200–2000 MNm². The disintegration time and dissolution rate of the different tablets were determined. Tablets formulated with gelatin or starch mucilage and compressed at 600 MNm² were selected for in vivo experiments using a urinary excretion method. Although both tablets complied with the disintegration requirements of the British Pharmacopoeia, dissolution rate and urinary excretion showed a difference in availability of drug from the two tablets.     

氯尼达明微粉化片剂的处方研究

目的:氯尼达明水溶性差,本文旨在研制其微粉化片剂处方并考察其稳定性.方法:使用球磨机制备氯尼达明微粉化混合物,并以此添加适合的辅料制备片剂.结果:经过溶出度试验,制剂达到了《中国药典》对溶出度的要求.初步稳定性研究表明,该制剂在60℃、相对湿度75%、4500Lax光照条件下10天稳定.结论:研制的氯尼达明片达到了设计要求.     

氯沙坦钾片剂的处方设计及其制备

目的:制备氯沙坦钾片.方法:分别考察稀释剂、崩解剂、黏合剂及包衣对氯沙坦钾片溶出度的影响.结果:采用乳糖、微晶纤维素为稀释剂,10%PVP为黏合剂,低取代羟丙基纤维素(L-HPC)为崩解剂,欧巴代包衣,制备的片剂溶出曲线与国外片基本相同.片剂外观优良,硬度适中,溶出性能良好.结论:该制备工艺操作简单、工艺成熟.     

The influence of excipients and technological process on cholecalciferol stability and its liberation from tablets.

The influence of excipients, used in tablet technology, and technological processes on cholecalciferol (1) stability was investigated. It was observed that 1 degrades in the presence of some excipients. The stability of 1 may be increased by antioxidant addition. The best stabilizing effect was achieved by a alpha-tocopherol and ascorbic acid mixture. On the basis of the achieved results, tablets with 1 were prepared. Their physical and chemical properties, the content of 1, its stability and its pharmaceutical availability were determined.     

咽炎咀嚼片的处方工艺研究

目的:研究咽炎咀嚼片的处方和工艺。方法:在单因素实验的基础上,采用正交试验设计,以多指标综合评分法对咽炎咀嚼片成型处方及工艺条件进行筛选。结果:优选的制剂处方为:咽炎粉50%、甘露醇35%、乳糖11%、枸橼酸1%、滑石粉1%、橙香精0.2%、阿司帕坦0.8%和硬脂酸镁l%。制得的咽炎咀嚼片表面光滑,色泽均一,硬度适中,口感良好。结论:该制备工艺简单,实用性强,所制备的咽炎咀嚼片质量符合相关要求。     

胆舒片处方工艺研究

目的对胆舒片进行处方工艺的筛选。方法以薄荷脑损耗率为指标,筛选处方工艺,并对优化处方工艺制备的胆舒片进行稳定性考察。结果按筛选出的最佳处方工艺制得的胆舒片含量合格、稳定,对光、热、湿敏感。结论该工艺有效地解决了薄荷脑稳定性问题,且制备工艺简单可行,适合工业化生产。     

Naproxen-Eudragit microspheres: screening of process and formulation variables for the preparation of extended release tablets

The objectives of the present study were to screen the formulation and process variables for the preparation of extended release naproxen tablets with Eudragit L100-55. The tablets were prepared by compression of microspheres that were obtained by a coprecipitation technique. The process involved dissolution of naproxen and Eudragit L 100-55 in alcohol USP followed by the addition of an aqueous solution containing a surfactant and deaggregating agents. The mixture was stirred for a specified time period to obtain microspheres, which were filtered and air-dried to a constant weight. The microspheres were then compressed to obtain plain tablets with a diameter of 12 mm. A 7-factor 12-run Plackett-Burman screening design was employed to evaluate the main effects of homogenization time (X1), rate of water addition (X2), amount of polymer (X3), amount of precipitating solution (X4), concentration of electrolytes (X5), compression pressure (X6), and the concentration of lubricant (X7) on the rate of drug release. The response variable was cumulative percent of naproxen dissolved in 12 h in simulated intestinal fluid with constraints on responses that included percent yield, hardness, thickness, and the angle of repose. Mathematical relationship for percent of naproxen dissolved in 12 h (Y5) with various factors yielded the following polynomial equation; Y5 (% dissolved in 12 h) = 95.48 + 0.53 X1 + 3.51 X2 + 3.84 X3 - 3.80 X4 - 2.46 X5 - 2.90 X6 - 3.91 X7. The results showed that all the seven factors affected, with varying order, the release of naproxen from its compressed tablets.     

头孢呋辛酯片处方研究及其溶出度考察

目的 通过对头孢呋辛酯片处方的改进来提高其溶出度.方法 通过不同组方筛选适宜的辅料和用量,并通过正交试验研究了微晶纤维素的用量、羧甲基淀粉钠的用量、粘合剂浓度对头孢呋辛酯片溶出度的影响.结果 微晶纤维素为110mg/片,羧甲基淀粉钠(CMS-Na)为15mg/片,聚维酮(PVP)为6%时,头孢呋辛酯片的溶出能达到中国药典2005年版附录对溶出度的要求.结论 采用合适的辅料与工艺,可显著地改善头孢呋辛酯片的溶出度.     

Influence of formulation and process variables on in vitro release of theophylline from directly-compressed Eudragit matrix tablets

Extended-release theophylline (TP) matrix tablets were prepared by direct compression of drug and different pH-dependent (Eudragit L100, S100 and L100-55) and pH-independent (Eudragit RLPO and RSPO) polymer combinations. The influence of varying the polymer/polymer (w/w) ratio and the drug incorporation method (simple blend or solid dispersion) was also evaluated. Drug release, monitored using the Through Flow Cell system, markedly depended on both the kind of Eudragit polymer combinations used and their relative content in the matrix. Maintaining a constant 1:1 (w/w) drug/polymers ratio, the selection of appropriate mixtures of pH-dependent and pH-independent polymers enabled achievement of a suitable control of TP release. In particular, matrices with a 0.7:0.3 w/w mixture of Eudragit L100-Eudragit RLPO showed highly reproducible drug release profiles, with an almost zero-order kinetic, and allowed 100% released drug after 360 min. As for the effect of the drug incorporation method, simple blending was better than the solid dispersion technique, which not only did not improve the release data reproducibility, but also caused, unexpectedly, a marked slowing down in drug release rate.     

处方和工艺因素对氨茶碱魔芋胶骨架片体外释放度的影响

目的：考察处方和工艺因素对魔芋胶骨架片体外释放度的影响，评价魔芋胶作为新型载体材料用于缓释骨架片制备的可行性。方法：以氨茶碱为模型药物，采用粉末直接压片法和湿法制粒压片法制备魔芋胶骨架片，考察魔芋胶粒度、黏度和用量，填充剂种类，主药粒度，压片工艺，压片压力等对其体外药物释放的影响。结果：氨茶碱魔芋胶骨架片可缓慢释放药物；随魔芋胶粒度降低，骨架材料用量或主药粒度增加，药物释放减慢；与淀粉、微晶纤维素和乳糖相比，Eudragit L100作为填充剂，可明显延缓药物释放；压片工艺，压片压力和魔芋胶黏度对药物释放影响不大。结论：魔芋胶可作为一种新型载体材料用于缓释骨架片的制备，魔芋胶粒度、用量，主药粒度和填充剂种类是影响骨架片体外药物释放的主要因素。     

利伐沙班片的制备及处方优化

目的：制备利伐沙班片剂,优选适合中试生产的最佳处方。方法通过设计不同处方,对增溶剂、崩解剂、黏合剂、填充剂的用量及工艺进行考察,并进行了中试三批放大,测定在四种溶出介质中的溶出曲线、含量均匀度和有关物质等指标。结果用利伐沙班为主药,以乳糖、微晶纤维素为填充剂,以十二烷基硫酸钠为增溶剂,以交联羧甲基纤维素钠为崩解剂,以羟丙基甲基纤维素为黏合剂、以硬脂酸镁为润滑剂,以胃溶型薄膜包衣预混剂为包衣材料,制得利伐沙班片。结论该制剂工艺稳定,制得利伐沙班片（10 mg）与原研市售品溶出行为相似,质量符合规定。